SKF-96365-hydrochloride - TRP Channel 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESKF-96365 hydrochlorideCat. No.: HY-100001CAS No.: 130495-35-1分式: CHClNO分量: 402.91作靶点: TRP Channel; Autophagy作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (248.19 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4819 mL 12.4097 mL 24.8194 mL5 mM 0.4964 mL 2.4819 mL 4.9639 mL10 mM 0.2482 mL 1.2410 mL 2.4819 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配

3、制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.20 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.20 mM); Clear solution3. 请依序

4、添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.20 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SKF-96365 hydrochloride选择性的TRP通道抑制剂。IC50 & Target TRP Channel 1体外研究 SKF-96365 exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and

5、 apoptosis in colorectalcancer cells. SKF-96365 inhibits hERG current in a concentration-dependent manner 1. SKF-96365 caninduces cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) fromthe mitochondria into the cytoplasm. Mechanistically, SKF-96365 treatmen

6、t inhibits the calcium/calmodulin-dependent protein kinase II (CaMKII)/AKT signaling cascade. Overexpression of CaMKII or AKTabolishes the effects of SKF-96365 on cancer cells, suggesting a critical role of the CaMKII/AKT signalingpathway in SFK-96365-induced biological effects 2.体内研究 SKF-96365 inhi

7、bits CRC cell growth in vivo. SKF-96365 treatment results in a decrease of p-CaMKII and p-AKT as well as an increase in LC3-II, cleaved PARP, caspase-3, and caspase-9 in mice 2.PROTOCOLAnimal Mice: Five to six-week-old female athymic BALB/c mice are inoculated into the right oxter with HCT116 cells.

8、Administration 2 When the diameter of the subcutaneous tumor reaches approximately 0.5 cm, animals are randomLyassigned to the vehicle, SKF-96365 alone, HCQ alone or SKF-96365+HCQ. SKF-96365 is applied (20mg/kg) and HCQ is applied (60 mg/kg) daily for 14 successive days by i.p. injection. Tumor size

9、s and volumeare determined. Eight mice are included in each group. Mice are sacrificed 24 h after the last treatment. Thetumors are weighed and processed for western blot analysis or paraffin embedding 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户

10、使本产品发表的科研献 FASEB J. 2019 Jun 5:fj201802550R. Acta Biochim Biophys Sin (Shanghai). 2019 Aug 5;51(8):767-777.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Liu H, et al. SKF-96365 blocks human ether-go-go-related gene potassium channels stably expressed in HEK 293 cells.Pharmaco

11、logical Research. Pharmacol Res, 2016 Feb, 104:61-9.2. Jing Z, et al. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of thecalcium/CaMKII/AKT-mediated pathway. Cancer Lett, 2016 Mar 28, 372(2):226-38.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: Product has not